Zhang, Xing Xing published the artcileDiscovery of 4-((E)-3,5-dimethoxy-2-((E)-2-nitrovinyl)styryl)aniline derivatives as potent and orally active NLRP3 inflammasome inhibitors for colitis, Name: 2-Methylbenzoic acid, the publication is European Journal of Medicinal Chemistry (2022), 114357, database is CAplus and MEDLINE.
A series of pterostilbene derivatives I [R1 = tert-Bu, Ph, 2-furyl, etc] were designed and synthesized based on previous SAR, leading to discovery of new effective NLRP3 inflammasome inhibitors with metabolic stability. Among them, the most effective compound I [R1 = 2-furyl] showed high inhibitory efficacy (against IL-1 ¦Â: IC50 = 1.23¦ÌM) and almost no toxicity (against IL-1 b: IC50 > 100¦ÌM). Further mechanism studies have showed that compound I [R1 = 2-furyl] directly targets the NLRP3 and affects the assembly of inflammasomes to inhibit the activation of NLRP3 inflammasomes. More importantly, in vitro experiments show that compound I [R1 = 2-furyl] has a significant therapeutic effect on DSS-induced colitis in mice with good metabolic stability to liver microsomes (t1/2 = 138.6 min). This research encourages the further development of more effective NLRP3 inflammasome inhibitors based on this chem. scaffold.
European Journal of Medicinal Chemistry published new progress about 118-90-1. 118-90-1 belongs to catalysis-chemistry, auxiliary class Carboxylic acid,Benzene,Natural product, name is 2-Methylbenzoic acid, and the molecular formula is C21H37BO, Name: 2-Methylbenzoic acid.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia